NADPH oxidase-IN-1 is an orally active NADPH oxidase ( Nox ) inhibitor, related with neuronal inflammation. NADPH oxidase-IN-1 can cross the blood-brain barrier (BBB), inhibits Nox2 and Nox4 with IC 50 s of 1.9 μM and 2.47 μM, respectively. NADPH oxidase-IN-1 suppresses pro-inflammatory cytokines production and LPS-mediated microglial migration, also has in vivo efficacy In Vitro NADPH oxidase-IN-1 (compound 11) can cross cross the blood-brain barrier (BBB) with P e value of 13.6 (10 -6 cm/s), determined by parallel artificial membrane permeability assay (PAMPA assay). NADPH oxidase-IN-1 (1 nM-10 mM; 30 min) LPS-induced ROS generation in BV2 microglial cells in a dose-dependent manner. NADPH oxidase-IN-1 (10 μM; 24 h) inhibits the mRNA expression of pro-inflammatory cytokines in BV2 cells. NADPH oxidase-IN-1 (1 nM-10 mM; 24 h) also inhibits activation and migration of BV2 cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only. RT-PCRCell Line: BV2 microglial cells Concentration: 10 μM Incubation Time: 24 hours Result: Inhibited the mRNA expression of pro-inflammatory cytokines (iNOS, IL-1β, TNFα) in BV2 cells. Cell Migration AssayCell Line: BV2 microglial cells Concentration: 10 μM Incubation Time: 24 hours Result: Ameliorated inflammatory response and migration of microglia. In Vivo NADPH oxidase-IN-1 (compound 11) (30 mg/kg; p.o.; daily for 4 wk) attenuates MPTP induced microglia activation and diminishes dopaminergic neuronal damage in Parkinson's disease (PD) mice model . NADPH oxidase-IN-1 is safe in both male and female mice following IV injection (10-300 mg/kg; single dose) and oral gavage (10-1000 mg/kg; single dose), respectively . Pharmacokinetic profile in rats Parameters C 0 (μg/mL) C max (μg/mL) t 1/2 (h) T max (h) AUC last (μg/h/mL) k e (1/h) V d (L) V d /F (L) Cl (L/h) Cl/F (L/h) F (%) IV (2 mg/kg) 1.70 0.79 0.468 1.32 0.211 0.217 PO (10 mg/kg) 0.609 5.01 [0.083-2] 1.31 0.170 1.99 0.341 56.0 PO (20 mg/kg) 0.783 6.13 [0.67-2] 4.16 0.159 1.82 0.217 88.9 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Form:Solid IC50& Target:NOX2 1.9 μM (IC 50 ) NOX4 2.47 μM (IC 50 )
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NADPH oxidase-IN-1
CAS number：2762405-17-2 molecular formula：C20H27N3O2S
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compound introduction
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| Chinese alias | NADPH 氧化酶-IN-1 | ||
| English alias | - | ||
| CAS number | 2762405-17-2 | molecular formula | C20H27N3O2S |
| molecular weight | 373.51 g/mol | Exact mass | - |
| PSA | - | logp | - |
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